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    • 6. 发明授权
    • 4-Tetrahydropyridylpyrimidine derivatives
    • 4-四氢吡啶基嘧啶衍生物
    • US06187781B1
    • 2001-02-13
    • US09381462
    • 1999-09-21
    • Atsuro NakazatoToshihito KumagaiTaketoshi OkuboIzumi AibeHideo TanakaShigeyuki ChakiShigeru OkuyamaKazuyuki Tomisawa
    • Atsuro NakazatoToshihito KumagaiTaketoshi OkuboIzumi AibeHideo TanakaShigeyuki ChakiShigeru OkuyamaKazuyuki Tomisawa
    • C07D40144
    • C07D401/04C07D405/14C07D409/14
    • A 4-tetrahydropyridylpyrimidine compound represented by formula (I): wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, and a trifluoromethyl group, a phenyl group, a thienyl group or a furanyl group; R1 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms; R2 represents an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, an alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms; and X1, X2, and X3, which may be the same or different, each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, an alkylthio group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof. The 4-Tetrahydropyridylpyrimidine compound finds utility in the treatment of diseases in which CRF is implicated.
    • 由式(I)表示的4-四氢吡啶基嘧啶化合物:其中Ar表示被1至3个选自卤素原子,具有1至5个碳原子的烷基,具有1至5个碳原子的烷氧基的取代基取代的苯基, 和三氟甲基,苯基,噻吩基或呋喃基; R1表示氢原子,碳原子数1〜5的烷基,氨基或被1〜2个碳原子数1〜2的烷基取代的氨基。 R2表示碳原子数1〜5的烷基,碳原子数4〜7的环烷基烷基,碳原子数2〜5的烯基或碳原子数2〜5的炔基。 X 1,X 2和X 3可以相同或不同,分别表示氢原子,卤素原子,碳原子数1〜5的烷基,碳原子数1〜5的烷氧基,烷硫基, 1至5个碳原子的氨基或被1或2个具有1至5个碳原子的烷基取代的氨基,或其药学上可接受的盐。 4-四氢吡啶基嘧啶化合物可用于治疗涉及CRF的疾病。
    • 8. 发明授权
    • Carbamoyl tetrahydropyridine derivatives
    • 氨基甲酰四氢吡啶衍生物
    • US06600038B1
    • 2003-07-29
    • US09914534
    • 2001-08-30
    • Atsuro NakazatoTaketoshi OkuboToshihito KumagaiKazuyuki Tomisawa
    • Atsuro NakazatoTaketoshi OkuboToshihito KumagaiKazuyuki Tomisawa
    • C07D47334
    • A61K31/519C07D473/00C07D487/04
    • Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
    • 由下式表示的氨基甲酰基四氢吡啶衍生物:[式中,R 1和R 2相同或不同,各自表示氢原子,C 1 -C 5烷基等; Y1-Y2表示(R4)C = C(R5),(R6)C = N,N = N,(R7)N-CO或N = C(R8) X1,X2和X3相同或不同,各自表示氢原子,卤素原子等; R3,R4,R5和R6相同或不同,各自表示氢原子或烷基; R7表示氢原子,C1-C5烷基等; 并且R8表示氢原子或氨基甲酰基]或其药学上可接受的盐,并且提供其制备的中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。
    • 9. 发明授权
    • Remedial agent for anxiety neurosis or depression and piperazine derivative
    • 焦虑神经症或抑郁症和哌嗪衍生物的补救剂
    • US06949552B2
    • 2005-09-27
    • US10311429
    • 2001-06-27
    • Atsuro NakazatoShigeyuki ChakiTaketoshi OkuboShin-ichi OgawaTakaaki Ishii
    • Atsuro NakazatoShigeyuki ChakiTaketoshi OkuboShin-ichi OgawaTakaaki Ishii
    • A61K31/495A61K31/496A61K45/06A61P25/22A61P25/24C07D295/125C07D401/06C07D403/06C07D413/14
    • C07D295/125A61K31/495A61K31/496A61K45/06C07C2601/02C07C2601/08C07C2601/14
    • There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by Formula [1]: [wherein Ar1 is a phenyl group, a substituted phenyl group, a naphthyl group or a substituted naphthyl group; Ar2 is a naphthyl group, a substituted naphthyl group, a quinolyl group, a group represented by the formula: (wherein R4 is a hydrogen atom or a halogen atom; and X—Y is CH—NH, CH—O, CH—S or N—O) or a group represented by the formula: (wherein R5 is a hydrogen atom, a hydroxyl group or a C1-10 alkoxy group); R1 is a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group, a C3-10 alkenyl group, a phenyl group, a 1-cyanoethyl group, a pyrimidin-2-yl group or an amidyl group; R2 and R3 are the same or different, and are each a hydrogen atom or a C1-10 alkyl group; A-B is N—CH2, CH—CH2, C(OH)—CH2 or C═CH; T1 is a single bond, —N(R6)— (wherein R6 is a hydrogen atom or a C1-10 alkyl group), —O—, —CH═CH— or —C(═O)—; n is an integer of from 1 to 10 and when T1 is a single bond, —CH═CH— or —C(═O)—, n is an integer of from 2 to 10 when T1 is —N(R6)— or —O—], or a pharmaceutically acceptable salt thereof.
    • 提供焦虑性神经症或抑郁症的治疗剂,其包含作为有效成分的MC 4受体拮抗剂; 和由式[1]表示的哌嗪衍生物:其中Ar 1是苯基,取代的苯基,萘基或取代的萘基; Ar 2是萘基,取代的萘基,喹啉基,由下式表示的基团:(其中R 4是氢原子或卤素原子; 并且XY是CH-NH,CH-O,CH-S或NO)或由下式表示的基团:(其中R 5是氢原子,羟基或C 1-10个烷氧基); R 1是氢原子,C 1-10烷基,C 3-8环烷基,C 3 -10个链烯基,苯基,1-氰基乙基,嘧啶-2-基或酰氨基; R 2和R 3相同或不同,并且各自为氢原子或C 1-10烷基; A-B是N-CH 2,CH-CH 2,C(OH)-CH 2或C-CH; T 1是单键,-N(R 6) - (其中R 6是氢原子或C 1 -10个烷基),-O - , - CH-CH-或-C( - O) - ; n是1〜10的整数,当T 1是单键时,-CH-CH-或-C(-O) - ,n是2〜10的整数,当T 或其药学上可接受的盐,其中R 1是-N(R 6) - 或-O-]。